Ha Eun-Sol, Baek In-hwan, Cho Wonkyung, Hwang Sung-Joo, Kim Min-Soo
College of Pharmacy, Pusan National University.
Chem Pharm Bull (Tokyo). 2014;62(6):545-51. doi: 10.1248/cpb.c14-00030.
The aim of the present study was to investigate the effect of Soluplus® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus® increases the aqueous solubility of atorvastatin calcium. Several solid dispersion formulations of atorvastatin calcium with Soluplus® were prepared at various drug : carrier ratios by spray drying. Physicochemical analysis demonstrated that atorvastatin calcium is amorphous in each solid dispersion, and the 2 : 8 drug : carrier ratio provided the highest degree of sustained atorvastatin supersaturation. Pharmacokinetic analysis in rats revealed that the 2 : 8 dispersion significantly improved the oral bioavailability of atorvastatin. This study demonstrates that spray-dried Soluplus® solid dispersions can be an effective method for achieving higher atorvastatin plasma levels.
本研究的目的是考察固体分散体辅料（Soluplus®）对阿托伐他汀钙溶解度的影响，并开发一种能提高阿托伐他汀钙口服生物利用度的固体分散体制剂。我们证明了Soluplus®可增加阿托伐他汀钙的水溶性。通过喷雾干燥法，以不同的药物∶载体比例制备了几种含Soluplus®的阿托伐他汀钙固体分散体制剂。物理化学分析表明，在每种固体分散体中阿托伐他汀钙均为无定形，且药物∶载体比例为2∶8时，阿托伐他汀的过饱和度维持程度最高。大鼠体内药代动力学分析表明，比例为2∶8的分散体显著提高了阿托伐他汀的口服生物利用度。本研究表明，喷雾干燥的Soluplus®固体分散体可能是实现更高阿托伐他汀血浆浓度的有效方法。
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